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Profile Name | FGFR3 over exp |
Gene Variant Detail | |
Relevant Treatment Approaches | FGFR Inhibitor (Pan) FGFR3 Antibody FGFR3 Inhibitor |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR3 Y373C FGFR3 over exp | multiple myeloma | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). | 22869148 |
FGFR3 K650E FGFR3 over exp HRAS K117E | myeloid neoplasm | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited Fgfr3 signaling and decreased proliferation of myeloma cells with HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). | 22869148 |
FGFR3 K650E FGFR3 over exp HRAS K117E | multiple myeloma | sensitive | PD173074 | Preclinical - Cell culture | Actionable | In a preclinical study, PD173074 inhibited Fgfr3 signaling, induced cell cycle arrest, and decreased proliferation of multiple myeloma cells harboring HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). | 22869148 |
FGFR3 Y373C FGFR3 over exp | multiple myeloma | sensitive | PD173074 | Preclinical | Actionable | In a preclinical study, PD173074 inhibited Fgfr3 signaling and decreased proliferation and survival of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). | 22869148 |
FGFR3 S249C FGFR3 over exp | transitional cell carcinoma | sensitive | PD173074 | Preclinical | Actionable | In a preclinical study, PD173074 inhibited growth of urothelial carcinoma (UC) cells expressing high levels of FGFR3 S249C, but had reduced efficacy against UC cells with low levels of FGFR3 S249C expression (PMID: 22869148). | 22869148 |
FGFR3 G384D FGFR3 over exp | multiple myeloma | decreased response | PD173074 | Preclinical | Actionable | In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to PD173074 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). | 22869148 |
FGFR3 G384D FGFR3 over exp | multiple myeloma | decreased response | AZD4547 | Preclinical | Actionable | In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZD4547 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). | 22869148 |
FGFR3 G384D FGFR3 over exp | multiple myeloma | decreased response | AZ8010 | Preclinical | Actionable | In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZ8010 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). | 22869148 |
FGFR3 mut FGFR3 over exp | urinary bladder cancer | sensitive | Dovitinib | Phase II | Actionable | In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 33% (1/3) of non-muscle invasive bladder cancer patients harboring both FGFR3 mutations and FGFR3 over expression (J Clin Oncol 34, 2016 (suppl; abstr 4526)). | detail... |
FGFR3 act mut FGFR3 over exp | transitional cell carcinoma | predicted - sensitive | Rogaratinib | Phase II | Actionable | In a Phase II trial (FORT-1), Rogaratinib (BAY 1163877) treatment resulted in a higher objective response rate of 52.4% (11/21) compared to 26.7% (4/15) with chemotherapy in advanced or metastatic urothelial carcinoma patients with FGFR3 overexpression and an FGFR3 alteration (including FGFR3 G370C, FGFR3 R248C, FGFR3 S249C, FGFR3 Y373C, FGFR3-TACC3v1, and FGFR3-TACC3v3) (PMID: 36240478; NCT03410693). | 36240478 |